不同类型的乳腺癌中，三阴性乳腺癌（TNBC）占乳腺恶性肿瘤的15％至20％。TNBC细胞的三个主要特征是（i）极端侵略性，（ii）缺乏激素和（iii）生长因子受体。由于缺乏或乙酰化的雌激素受体，人类表皮生长因子受体2和孕激素受体，TNBC对激素和内分泌治疗具有抗性。因此，目前的主要方法是使用化疗来对抗TNBC。已经观察到癌细胞中雄激素受体（AR）在部分TNBC患者中的表达。因此，抑制雄激素信号通路为针对TNBC提供了希望。新的AR抑制剂打开了针对携带AR阳性TNBC细胞的乳腺癌患者的新疗法可能性。我们小组提供了AR结构和功能的综合评估以及针对TNBC细胞核受体的临床证据。我们更新了AR激动剂、抑制剂和拮抗剂。我们还提出了基因测序的新时代CRISPR / Cas9和纳米技术作为AR最先进的方法以促进TNBC中靶向治疗的效率。 意义陈述：三阴性乳腺癌的有效治疗缺乏是一个健康挑战。现有治疗的主要缺点是由于其非特异性靶向而引起的副作用。分子靶向细胞受体，如雄激素受体，增加在恶性组织中的表达，显着提高乳腺癌患者的生存率。版权所有©美国药理学和实验治疗协会2023年。

Among different types of breast cancers (BC), triple-negative BC (TNBC) amounts to 15% to 20% of breast malignancies. Three principal characteristics of TNBC cells are (i) extreme aggressiveness, (ii) absence of hormones, and (iii) growth factor receptors. Due to the lack or poor expression of the estrogen receptor, human epidermal growth factor receptor 2, and progesterone receptor, TNBC is resistant to hormones and endocrine therapies. Consequently, chemotherapy is currently used as the primary approach against TNBC. Expression of androgen receptor (AR) in carcinoma cells has been observed in a subset of patients with TNBC; therefore, inhibiting androgen signaling pathways holds promise for TNBC targeting. The new AR inhibitors have opened up new therapy possibilities for BC patients carrying AR-positive TNBC cells. Our group provides a comprehensive review of the structure and function of the AR and clinical evidence for targeting the cell's nuclear receptor in TNBC. We updated AR agonists, inhibitors, and antagonists. We also presented a new era of genetic manipulating CRISPR/Cas9 and nanotechnology as state-of-the-art approaches against AR to promote the efficiency of targeted therapy in TNBC. SIGNIFICANCE STATEMENT: The lack of effective treatment for triple-negative breast cancer is a health challenge. The main disadvantages of existing treatments are their side effects, due to their nonspecific targeting. Molecular targeting of cellular receptors, such as androgen receptors, increased expression in malignant tissues, significantly improving the survival rate of breast cancer patients.Copyright © 2023 by The American Society for Pharmacology and Experimental Therapeutics.